阿霉素与Annexin V的偶联及其对乳腺癌细胞的杀伤作用

目的研究将阿霉素与Annexin V偶联的方法,以及偶联物对乳腺癌细胞的杀伤作用。方法使用EDC/sulfo-NHS为偶联剂,将阿霉素与Annexin V偶联,使用紫外可见分光光度法对偶联物进行了表征,用MTT方法检测偶联物对过氧化氢处理的乳腺癌细胞系MDA-MB-231的肿瘤细胞杀伤作用。结果在过量的EDC存在下,提高sulfo-NHS的浓度,有助于提高偶联比。偶联物的浓度为1μmol/L时,MDA-MB-231肿瘤细胞的存活率只有27.7%;而单独使用阿霉素,浓度要达到1.8μmol/L时,才能达到相同的抑制率;Annexin V在3.88μmol/L时,细胞存活率为63.9%。结论偶联物对MDA-MB-231肿瘤细胞的杀伤作用要强于两者分别单独使用时的效果,这为进一步研究抗肿瘤药物提供了依据。

Conjugation of Doxorubicin with Annexin V and its cytotoxic function on tumor cell line MDA-MB-231 cell line

Purpose To investigate a method by which Doxorubicin(Dox)-Annexin V conjugate was synthesized and cytotoxicity activity of the conjugate to breast cancer cell.Methods Using EDC/sulfo-NHS as coupling reagent,a Dox-Annexin V conjugate was synthesized.The conjugate was characterized using spectrophotometry.Cytotoxicity activity of the conjugate to MDA-MB-231 cell line treated with H2O2 was measured using MTT method.Results If EDC was excessive the increasing concentration of sulfo-NHS can raise molar ratio(moles of Dox/moles of Annexin V) of the conjugate.When the conjugate was applied at concentration of 1 μmol/L,survival rate of MDA-MB-231 cells was 27.7%.But to achieve the similar inhibition result,Dox needed to be used at a concentration of 1.8 μmol/L.When Annexin V was used at concentration of 3.88 μmol/L,cellular survival rate was 63.9%.Conclusion Cytotoxicity activity of the conjugate to MDA-MB-231 was superior to either Dox or Annexin V.This result provided foundations for further study.